posted on 2004-09-23, 00:00authored byMichael L. Miller, Elizabeth E. Roller, Robert Y. Zhao, Barbara A. Leece, Olga Ab, Erkan Baloglu, Victor S. Goldmacher, Ravi V. J. Chari
To develop effective taxane−antibody immunoconjugates, we have prepared a series of modified taxanes that
have both improved toxicity and solubility in aqueous systems
as compared to paclitaxel (1a). These taxanes have been
modified at either the C-10 or C-7 position and were found to
be very cytotoxic against both normal and multi-drug-resistant
(MDR) cells, as well as up to 30 times more soluble than
paclitaxel in various buffer systems.